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Glucose sensitive controlled release microballoon composition and preparation method thereof

A composition and microsphere technology, which can be applied in the directions of drug combination, medical preparations with non-active ingredients, non-active ingredients of polymer compounds, etc. Effect

Active Publication Date: 2015-07-01
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention provides a sugar-sensitive sustained and controlled-release microsphere composition, which solves the problem that traditional drugs for treating diabetes cannot self-regulate and release diabetes drugs according to changes in blood sugar in the body

Method used

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  • Glucose sensitive controlled release microballoon composition and preparation method thereof
  • Glucose sensitive controlled release microballoon composition and preparation method thereof
  • Glucose sensitive controlled release microballoon composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Weigh 250 mg of ketal polymer material with a molecular weight of 4200, 6 mg of glucose oxidase, and 6 mg of catalase, add 2 mL of dichloromethane to dissolve, and form a homogeneous suspension as the oil phase; 12 mg of bovine insulin is dissolved in 50 μL of DMSO As a drug solution; put the oil phase in a homogenizer (IKA T25, Staufenim Breisgau, Germany) at 7500r min -1 Under homogeneous conditions, the drug solution was dropped into the oil phase, and the anti-solvent effect caused the precipitation of insulin to form a uniform S / O suspension, which continued to be homogenized for 2 minutes; -1Drop into 66mL PVA aqueous solution with a concentration of 10mg / ml under magnetic stirring conditions to form S / O / W double emulsion; stir at low speed, volatilize the organic solvent for 8 hours, and solidify the microspheres; pass through a 1200-mesh sieve and deionize at 0°C The microspheres were washed with water for 3 times, transferred to a petri dish, and freeze-dri...

Embodiment 2

[0043] Weigh 250 mg of ketal polymer material with a weight average molecular mass of 4200, 24 mg of glucose oxidase, and 24 mg of catalase, add 2 mL of dichloromethane to dissolve, and form a homogeneous suspension as the oil phase; 12 mg of bovine insulin is dissolved in 50 μL of DMSO was used as a drug solution; the oil phase was placed in a homogenizer (IKA T25, Staufenim Breisgau, Germany), at 25000r min -1 The drug solution was dropped into the oil phase under homogeneous conditions, and the anti-solvent effect caused insulin to precipitate to form a uniform S / O suspension, which lasted for 2 minutes; the above solution was dropped into the oil phase under the condition of 1500r·min-1 magnetic stirring Form S / O / W double emulsion in 50mL of PVA aqueous solution with a concentration of 10mg / ml; stir in an ice-water bath at low speed for 8h, volatilize the organic solvent, and solidify the microspheres; pass through a 1200-mesh sieve, and wash the microspheres with deio...

Embodiment 3

[0045] Weigh 100 mg of ketal polymer material with a weight average molecular weight of 2200, 6 mg of glucose oxidase, and 6 mg of catalase, add 2 mL of dichloromethane to dissolve, and form a homogeneous suspension as the oil phase; 12 mg of bovine insulin is dissolved in 50 μL of In DMSO as a drug solution; the oil phase is placed in a homogenizer, at 13000r min -1 The drug solution was dropped into the oil phase under homogeneous conditions, and the anti-solvent effect caused insulin to precipitate to form a uniform S / O suspension, which lasted for 2 minutes; the above solution was dropped into the oil phase under the condition of 1500r·min-1 magnetic stirring Form S / O / W double emulsion in 118mL PVA aqueous solution with a concentration of 10mg / ml; stir in an ice-water bath at low speed for 8h, volatilize the organic solvent, and solidify the microspheres; pass through a 1200-mesh sieve, and wash the microspheres with deionized water at 0°C 3 times, transferred to a petri d...

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Abstract

The invention discloses a glucose sensitive controlled release microballoon composition and a preparation method thereof. The medicine for treating the diabetes, the glucose oxidase (GOD) and the catalase (POD) are embedded in the microballoon. By taking the insulin as an example, when the in-vivo glucose concentration is raised, the glucose can be diffused to the surface of the microballoon and is oxidized by the GOD in the microballoon to form the gluconic acid, the pH value in the environment is reduced to about 3-5, the microballoon degradation and corrosion speed is rapidly increased and the insulin release speed is quickened; when the blood sugar concentration is controlled, the PH value is recovered to the physiological PH value of about 7.4, the microballoon degradation speed is reduced and the insulin release speed is slowed. When the blood sugar is raised again, the release behavior is repeated, the insulin presents a glucose-sensitive self-regulating release behavior, the POD can perform catalytic decomposition on the hydrogen peroxide to generate oxygen, the oxygen consumed in the microballoon GOD enzyme reaction is compensated and the enzyme active utilization rate is increased. The glucose sensitive controlled release microballoon composition can be used for solving the problem that the traditional medicine for treating the diabetes cannot perform self regulation to release the diabetes treating medicine according to the in-vivo blood sugar change.

Description

technical field [0001] The invention relates to a sugar-sensitive sustained and controlled release microsphere composition and a preparation method thereof, which is a microsphere composition for regulating drug release based on a macromolecule degradation and erosion mechanism, and belongs to the technical field of pharmaceutical production. Background technique [0002] Diabetes is a chronic disease that seriously endangers human health. With the improvement of people's living standards, the aging population and the increase in the incidence of obesity, the incidence of diabetes is increasing year by year. Research shows that the incidence of diabetes in my country has reached 9.7% in 2010, and the trend of younger people is becoming more and more obvious. Diagnosed in 2013 according to the latest international clinical diagnostic criteria, the estimated prevalence rate of diabetes among adults aged 18 and over in my country was 11.6%. If diabetes is not treated in time, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/34A61K9/16A61K9/19A61K9/113A61P3/10A61K38/22A61K38/28A61K31/64A61K31/155
Inventor 孙考祥张峰溥王正
Owner YANTAI UNIV
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